Donepezil HCl

SKU: orb1300734

Description

Donepezil HCl (Aricept) is a potent and selective acetylcholinesterase (AChE) inhibitor, effective against both bovine and human enzymes with IC50 values in the low nanomolar range. It is widely used in neuroscience research for in vitro enzymatic assays and in vivo studies related to cholinergic function and cognitive models.

Research Area

Cardiovascular Research, Cell Biology, Neuroscience

Key Properties

• CAS Number: 120011-70-3
• MW: 416.0
• Purity: >98%
• Formula: C₂₄H₂₉NO₃ • HCl
• SMILES: Cl.COc1c(OC)cc2C(=O)C(CC3CCN(Cc4ccccc4)CC3)Cc2c1
• Target: Acetylcholinesterase/Butyrylcholinesterase
• Solubility: Soluble in DMSO (up to 20 mg/ml) or in Water (up to 20 mg/ml).

Bioactivity

• Target IC50:
  AChE (human):11.6 nM|AChE (bovine):8.12 nM
• In Vivo:
  Intraperitoneal administration of Donepezil in rats produces a dose dependent increase in salivation and tremor, which are overt cholinergic behavioural signs, with an ED50 of 6 μmol/kg. Donepezil is found to be somewhat less potent with a ED50 of 50 μmol/kg following oral administration. . When administered separately in vivo, 5-HT(4) receptor inducer, RS67333 (0.3 and 1 mg/kg) and Donepezil (1 mg/kg) improves recognition performances compared to saline treated mice, while co-administration of subactive doses of RS67333 (0.1 mg/kg) and Donepezil (0.3 mg/kg) improves memory. However, this improvement is prevented if a 5-HT(4)R antagonist (GR125487, 10 mg/kg) is also administered.
• In Vitro:
  Donepezil inhibits the carbachol-stimulated increase in intracellular Ca2+ concentration in human SHSY5Y neuroblastoma cells in a concentration dependent manner, indicating that Donepezil have muscarinic antagonist activity. A recent study shows that Donepezil can protect human umbilical vein endothelial cells (HUVECs) against Water2-induced cell injury. This may be useful as a potential therapy for oxidative stress in cardiovascular and cerebrovascular diseases.

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E-2020

Compound Identifiers

PubChem CID

5741